Xeloda

Xeloda (capecitabine) is an innovative oral chemotherapeutic agent that offers a targeted approach to treating specific advanced cancers. As a prodrug, it is selectively converted to its active form—5-fluorouracil (5-FU)—primarily within tumor tissue, maximizing anticancer activity while potentially reducing systemic exposure. This mechanism allows for convenient at-home administration, providing a flexible and patient-centered treatment option. Xeloda is commonly used in monotherapy or combination regimens for colorectal, breast, and gastric cancers, supported by robust clinical evidence demonstrating efficacy and manageable tolerability.

Features

• Oral tablet formulation in 150 mg and 500 mg strengths
• Prodrug selectively activated to 5-fluorouracil by thymidine phosphorylase in tumor cells
• Dosing regimen typically involves two weeks of treatment followed by one week of rest
• Bioavailability of nearly 100% when taken with food
• Metabolized primarily in the liver and activated in tumor tissues

Benefits

• Enables convenient outpatient treatment without frequent clinic visits for intravenous administration
• Provides targeted delivery of chemotherapy directly to cancer cells, potentially reducing impact on healthy tissues
• Demonstrates proven efficacy in metastatic colorectal cancer, both as monotherapy and in combination regimens
• Offers flexible dosing that can be adjusted based on individual tolerance and response
• Supported by extensive clinical data establishing its role in adjuvant and metastatic settings
• May improve quality of life by allowing treatment continuity outside clinical settings

Common use

Xeloda is indicated for:

• Adjuvant treatment of Dukes’ C colon cancer following complete resection of the primary tumor
• First-line treatment of metastatic colorectal cancer
• Treatment of metastatic breast cancer either as monotherapy or in combination with docetaxel, following failure of prior anthracycline-containing chemotherapy
• First-line treatment of advanced gastric cancer in combination with platinum-based chemotherapy

Dosage and direction

The recommended dosage of Xeloda is 1250 mg/m² administered orally twice daily (morning and evening) for 2 weeks followed by a 1-week rest period, given as 3-week cycles. Tablets should be taken within 30 minutes after a meal with water. Dosage adjustments are based on body surface area and should be individualized according to toxicity and tolerance. For patients with renal impairment, dose reduction is recommended. Treatment should continue until disease progression or unacceptable toxicity occurs.

Precautions

• Monitor patients for diarrhea, which can be severe and lead to dehydration and renal impairment
• Regular assessment of cardiac function is recommended due to potential cardiotoxicity
• Patients with dihydropyrimidine dehydrogenase (DPD) deficiency may experience severe toxicity
• Monitor for hand-foot syndrome (palmar-plantar erythrodysesthesia), which may require dose modification
• Regular complete blood counts and liver function tests are recommended during treatment
• Use with caution in elderly patients due to increased incidence of adverse reactions
• Advise patients to avoid sunlight exposure due to increased photosensitivity

Contraindications

• Known hypersensitivity to capecitabine, 5-fluorouracil, or any component of the formulation
• Patients with known complete deficiency of dihydropyrimidine dehydrogenase (DPD) activity
• Severe renal impairment (creatinine clearance below 30 mL/min)
• Pregnancy and breastfeeding
• Concurrent administration with sorivudine or its chemically related analogues

Possible side effect

Common adverse reactions (≥10%):

• Diarrhea (47%)
• Hand-foot syndrome (54%)
• Nausea (34%)
• Vomiting (15%)
• Fatigue (16%)
• Stomatitis (22%)
• Anorexia (13%)
• Hyperbilirubinemia (22%)

Serious side effects requiring immediate medical attention:

• Severe diarrhea leading to dehydration
• Cardiotoxicity including myocardial infarction, angina, and arrhythmias
• Severe hand-foot syndrome requiring dose interruption
• Neutropenia and thrombocytopenia
• Severe hyperbilirubinemia
• Dizziness and headache

Drug interaction

• Warfarin: Increased anticoagulant effect and risk of bleeding; frequent INR monitoring required
• Phenytoin: Increased phenytoin levels and risk of toxicity
• Leucovorin: Enhanced toxicity without evidence of increased efficacy
• Allopurinol: May decrease efficacy of Xeloda
• Antacids: Aluminum hydroxide and magnesium hydroxide may increase capecitabine concentrations
• CYP2C9 substrates: Potential interactions with drugs metabolized by this enzyme

Missed dose

If a dose is missed, do not take the missed dose at the next scheduled time. Resume the regular dosing schedule with the next prescribed dose. Do not double the dose to make up for a missed dose. Contact your healthcare provider for specific guidance if multiple doses are missed.

Overdose

Overdose may manifest as nausea, vomiting, diarrhea, gastrointestinal irritation and bleeding, bone marrow depression, and acute renal failure. There is no specific antidote for Xeloda overdose. Treatment should consist of general supportive measures, including hydration and monitoring of hematological parameters. Hemodialysis may be considered, though its effectiveness in removing capecitabine and its metabolites is limited.

Storage

Store at room temperature (20-25°C or 68-77°F) in the original container with the lid tightly closed. Keep away from moisture and light. Do not store in bathroom or kitchen cabinets where humidity levels may be higher. Keep out of reach of children and pets. Do not use after the expiration date printed on the packaging.

Disclaimer

This information is provided for educational purposes only and does not constitute medical advice. Treatment decisions should be made in consultation with a qualified healthcare professional familiar with the individual patient’s medical history and current condition. Dosage and administration may vary based on specific clinical circumstances. Always follow the prescribing information provided by the manufacturer and the guidance of your treating physician.

Reviews

Clinical studies demonstrate that Xeloda shows comparable efficacy to intravenous 5-FU/leucovorin in metastatic colorectal cancer, with response rates of approximately 25-35% as monotherapy. In breast cancer, combination therapy with docetaxel shows response rates of 42-55%. The convenience of oral administration is frequently cited as significantly improving quality of life compared to intravenous regimens. However, hand-foot syndrome and gastrointestinal toxicity remain notable management challenges that require careful dose modification and supportive care.